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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 408025Generated: October 26, 2026

Trifluoroacetic acid → (3S)-1-(3,3-dimethylpiperidin-4-yl)-3-(2-fluoro-4-(methylsulfonyl)phenylamino)pyrrolidin-2-one

https://huagongshe.com/reaction/408025

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
Reactanttert-butyl 4-((S)-3-(2-fluoro-4-(methylsulfonyl)phenylamino)-2-oxopyrrolidin-1-yl)-3,3-dimethylpiperidine-1-carboxylateHCID 67469764—
SolventDichloromethaneHCID 6344—
Product(3S)-1-(3,3-dimethylpiperidin-4-yl)-3-(2-fluoro-4-(methylsulfonyl)phenylamino)pyrrolidin-2-oneHCID 6746973625%

Reaction Steps

tert-Butyl 4-((S)-3-(2-fluoro-4-(methylsulfonyl)phenylamino)-2-oxopyrrolidin-1-yl)-3,3-dimethylpiperidine-1-carboxylate (0.10 g, 0.21 mmol) was dissolved in DCM (5 mL). TFA (5 mL) was added and the reaction was stirred for 1 hour. The solution was concentrated, neutralized with saturated NaHCO3 solution, and extracted with dichloromethane (3 times). The organic layers were combined, dried, filtered and concentrated to give (3S)-1-(3,3-dimethylpiperidin-4-yl)-3-(2-fluoro-4-(methylsulfonyl)phenylamino)pyrrolidin-2-one (0.020 g, 0.052 mmol, 25% yield) as a white solid.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08754226B2
Source datasetuspto-grants-2014_06
ORD IDord-e427cfe33da84a469938b7acff1f2fc7
Source noteuspto-grants-2014_06